头孢氨苄 - CAS号 23325-78-2

物化性质

熔点：

>161°C (dec.)
溶解度：

NH4OH1M:50 mg/mL,透明,黄色
颜色/状态：

CRYSTALS
稳定性/保质期：
解离常数：

PKA: 5.2, 7.3

计算性质

辛醇/水分配系数(LogP)：

-0.38
重原子数：

25
可旋转键数：

4
环数：

3.0
sp3杂化的碳原子比例：

0.31
拓扑面积：

139
氢给体数：

4
氢受体数：

7

ADMET

毒理性

在妊娠和哺乳期间的影响

◉ 母乳喂养期间使用总结：有限的信息表明，母体服用头孢氨苄会在乳汁中产生较低水平，通常不会预期对哺乳婴儿造成不良影响。头孢氨苄是治疗乳腺炎的一种替代药物。偶尔会有报道指出，婴儿的胃肠道菌群受到干扰，导致腹泻或鹅口疮，但这些效果尚未得到充分评估。在一例罕见病例中，一名之前接触过静脉注射头孢唑啉的婴儿，在母亲开始服用头孢氨苄时出现了严重的过敏反应。头孢氨苄在哺乳母亲中是可以接受的。 ◉ 对哺乳婴儿的影响：在一项前瞻性随访研究中，7位哺乳母亲报告服用头孢氨苄（剂量未指定）。其中两位母亲报告其婴儿出现腹泻。没有报道暴露的婴儿出现皮疹或念珠菌病。在一项前瞻性、对照研究中，询问了拨打信息服务电话的母亲关于其哺乳婴儿的不良反应经历。11名暴露于头孢氨苄的婴儿中，据报道有一名在母亲服用头孢氨苄治疗期间出现了腹泻。一名妇女接受静脉注射头孢噻吩1克，每6小时一次，共3天。她的哺乳婴儿出现绿色液体粪便、严重腹泻、不适和哭闹。随后，母亲的用药方案改为口服头孢氨苄500毫克加口服丙磺舒500毫克，每日四次，持续16天。在此期间，婴儿继续腹泻。作者认为腹泻可能与乳汁中的头孢氨苄有关。一名4个月大的婴儿因尿路感染接受静脉注射头孢唑啉治疗。出院并停用头孢唑啉9天后，婴儿大部分身体出现水疱性皮疹，被诊断为中毒性表皮坏死松解症（TEN）。婴儿的母亲在症状出现前2天开始服用头孢氨苄，并正在哺乳（程度未指定）。在TEN治疗完成后4周进行的淋巴细胞转化测试发现对头孢唑啉和头孢氨苄都有致敏反应。婴儿的反应可能是由乳汁中的头孢氨苄引起的，在初次致敏后，随后对头孢唑啉产生交叉反应。 ◉ 对泌乳和乳汁的影响：截至修订日期，未找到相关已发布信息。

◉ Summary of Use during Lactation:Limited information indicates that maternal cephalexin produces low levels in milk that are usually not expected to cause adverse effects in breastfed infants. Cephalexin is an alternative for the treatment of mastitis. Occasionally disruption of the infant's gastrointestinal flora, resulting in diarrhea or thrush have been reported with cephalosporins, but these effects have not been adequately evaluated. A rare case of a severe allergic reaction occurred in an infant previously exposed to intravenous cefazolin whose mother began taking cephalexin while breastfeeding. Cephalexin is acceptable in nursing mothers. ◉ Effects in Breastfed Infants:In a prospective follow-up study, 7 nursing mothers reported taking cephalexin (dosage not specified). Two mothers reported diarrhea in their infants. No rashes or candidiasis were reported among the exposed infants. A prospective, controlled study asked mothers who called an information service about adverse reactions experience by their breastfed infants. One of 11 cephalexin-exposed infants reportedly developed diarrhea during maternal cephalexin therapy. A woman received intravenous cephalothin 1 g every 6 hours for 3 days. Her breastfed infant had a green liquid stool, severe diarrhea, discomfort and crying. The mother's drug regimen was then changed to oral cephalexin 500 mg plus oral probenecid 500 mg 4 times daily for another 16 days. The infant continued to have diarrhea during this time. The authors rated the diarrhea as probably related to cephalexin in milk. A 4-month-old infant was treated with intravenous cefazolin for a urinary tract infection. Nine days after being discharged and cefazolin discontinuation, the infant developed a blistering rash over most of the body that was diagnosed as toxic epidermal necrolysis (TEN). The infant was being breastfed (extent unspecified) by his mother who had begun cephalexin 2 days prior to the onset of symptoms. A lymphocyte transformation test performed 4 weeks after treatment for TEN was completed found sensitization to both cefazolin and cephalexin. The infant's reaction was probably caused by cephalexin in breastmilk after initial sensitization and subsequent cross-reaction to cefazolin. ◉ Effects on Lactation and Breastmilk:Relevant published information was not found as of the revision date.

来源:Drugs and Lactation Database (LactMed)

毒理性

相互作用

利尿剂苯溴马隆（Probenecid）能有效减缓尿液清除速度并增强头孢氨苄（Cephalexin）的系统抗菌活性持续时间。

PROBENECID IS EFFECTIVE IN SLOWING URINARY CLEARANCE & ENHANCING DURATION OF SYSTEMIC ANTIMICROBIAL ACTIVITY /OF CEPHALEXIN/.